Montiget

Montiget Chewable Tablets 5 mg: Each tablet contains Montelukast sodium equivalent to Montelukast 5 mg.
Montiget Tablets 10 mg: Each tablet contains Montelukast sodium equivalent to Montelukast 10 mg.

Pharmacology: Pharmacodynamics: Montelukast is an orally active compound that binds with high affinity and selectivity to the CysLT type-1 (CysLT₁) receptor. Montelukast inhibits physiologic actions of LTD₄ at the CysLT₁ receptor without any agonist activity. The cysteinyl leukotrienes (LTC₄, LTD₄, LTE₄) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to CysLT receptors. Cysteinyl leukotriene production and receptor occupation have been correlated with the pathophysiology of allergic rhinitis and asthma. The CysLT₁ receptor is found in the human airway (including airway smooth muscle cells and airway macrophages) and on other proinflammatory cells (including eosinophils and certain myeloid stem cells).
Pharmacokinetics: Absorption: Montelukast is rapidly absorbed following oral administration. After administration of the 10 mg film-coated tablet to fasted adults, the mean peak montelukast plasma concentration (C_max) is achieved in 3 to 4 hours (T_max). The mean oral bioavailability is 64%. The oral bioavailability and C_max are not influenced by a standard meal in the morning.
For the 5 mg chewable tablet, the mean C_max is achieved in 2 to 2.5 hours after administration to adults in the fasted state. The mean oral bioavailability is 73% in the fasted state versus 63% when administered with a standard meal in the morning.
For the 4 mg chewable tablet, the mean C_max is achieved 2 hours after administration in pediatric patients 2 to 5 years of age in the fasted state.
Distribution: Montelukast is more than 99% bound to plasma proteins. The steady state volume of distribution of montelukast averages 8 to 11 liters.
Metabolism: Montelukast is extensively metabolized. In studies with therapeutic doses, plasma concentrations of metabolites of montelukast are undetectable at steady state in adults and pediatric patients. In vitro studies using human liver microsomes indicate that CYP3A4, 2C8, and 2C9 are involved in the metabolism of montelukast. At clinically relevant concentrations, 2C8 appears to play a major role in the metabolism of montelukast.
Excretion: The plasma clearance of montelukast averages 45 mL/min in healthy adults. Montelukast and its metabolites are excreted almost exclusively via the bile. The mean plasma half-life of montelukast ranged from 2.7 to 5.5 hours in young adults. The pharmacokinetics of montelukast are nearly linear for oral doses up to 50 mg. During once-daily dosing with 10 mg montelukast, there is little accumulation of the parent drug in plasma (14%).
Special Populations: Hepatic function impairment: In patients with mild to moderate hepatic insufficiency and cirrhosis, metabolism was decreased, resulting in a 41% higher mean AUC. The elimination is prolonged with a mean half-life of 7.4 hours.
Elderly: The plasma half-life of montelukast is slightly longer in elderly patients.
Children: In children 6 to 11 months of age, the systemic exposure and the variability of plasma montelukast concentrations are higher than those observed in adults. Mean AUC (4296 ng•hr/mL) was 60% higher and the mean C_max (667 ng/mL) was 89% higher than those observed in adults. The systemic exposure in children 12 to 23 months of age was less variable, but was still higher than that observed in adults. The mean AUC (3,574 ng•hr/mL was 33% higher and the mean C_max (562 ng/mL) was 60% higher than those observed in adults.

MONTIGET is indicated in adult and pediatric patients 6 years of age and older for the prophylaxis and chronic treatment of asthma, including the prevention of day- and nighttime symptoms, the treatment of aspirin-sensitive asthmatic patients, and the prevention of exercise-induced bronchoconstriction.
MONTIGET is indicated for the relief of daytime and nighttime symptoms of allergic rhinitis (seasonal allergic rhinitis in adults and pediatric patients 6 years of age and older, and perennial allergic rhinitis in adults and pediatric patients 6 years of age and older).

Recommended Dose: For mild persistent asthmatic, it should be taken once daily. For moderate to severe asthma, it should be taken once daily concomitantly with inhaled corticosteroids to provide additional benefit. The dose should be taken in the evening.
For allergic rhinitis, it should be taken once daily. In patients who are not adequately controlled on the standard therapy according to specialized physicians' consideration, concomitant administration of MONTIGET may result in further improvement of symptoms. The time of administration may be individualized to suit patient needs.
Patients with both asthma and allergic rhinitis should take only one tablet daily in the evening.
Adults and children 15 years and older with Asthma and/or Allergic Rhinitis: The dosage for adults 15 years of age and older is one 10-mg tablet once daily.
Pediatric Patients 6 to 14 years of age with Asthma and/or Allergic Rhinitis: The dosage for pediatric patients 6 to 14 years of age is one 5-mg chewable tablet daily.
No dosage adjustment is necessary for pediatric patients, for the elderly, for patients with renal insufficiency, or mild-to-moderate hepatic impairment, or for patients of either gender.
Mode of Administration: It may be administered orally without regard to food or meals. Patients should be advised to continue taking this drug while their asthma is controlled, as well as during periods of worsening asthma.
Therapy with MONTIGET in Relation to Other Treatments for Asthma: MONTIGET can be added to a patient's existing treatment regimen.
Reduction in Concomitant Therapy: Bronchodilator Treatments: MONTIGET can be added to the treatment regimen of patients who are not adequately controlled on bronchodilator alone. When a clinical response is evident (usually after the first dose), the patient's bronchodilator therapy can be reduced as tolerated.
Inhaled Corticosteroids: Treatment with MONTIGET provides additional clinical benefit to patients treated with inhaled corticosteroids. A reduction in the corticosteroid dose can be made as tolerated. The dose should be reduced gradually with medical supervision. In some patients, the dose of inhaled corticosteroids can be tapered off completely. MONTIGET should not be abruptly substituted for inhaled corticosteroids.

Symptoms: There have been reports of acute overdosage in post marketing experience and clinical studies with montelukast. These include reports in adults and children with a dose as high as 1000 mg. The clinical and laboratory findings observed were consistent with the safety profile in adults and pediatric patients. There were no adverse experiences in the majority of overdosage reports. The most frequently occurring adverse experiences were consistent with the safety profile of montelukast sodium and included abdominal pain, somnolence, thirst, headache, vomiting, and psychomotor hyperactivity.
Treatment: No specific information is available on the treatment of overdose with montelukast. In the event of overdose, it is reasonable to employ the usual supportive measures; eg, remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring, and institute supportive therapy, if required. It is not known whether montelukast is removed by peritoneal dialysis or hemodialysis.

Hypersensitivity to montelukast or any component of the formulation.

Acute asthma attacks: Montelukast is not indicated for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus. Continue therapy during acute exacerbations of asthma. Advise patients to have appropriate rescue medication available.
CNS effects: Neuropsychiatric events have been reported in adults, adolescent, and pediatric patients taking leukotriene modifiers. Agitation, aggressive behavior or hostility, anxiousness, depression, disorientation, disturbance in attention, dream abnormalities, hallucinations, insomnia, irritability, memory impairment, restlessness, somnambulism, suicidal thinking and behavior (including suicide) and tremor have been reported postmarketing. Be alert for neuropsychiatric events and instruct patients to report the occurrence of these changes. Carefully evaluate the risks and benefits of continuing treatment if such events occur.
Eosinophilic conditions: Patients receiving montelukast may present with systemic eosinophilia, eosinophilic pneumonia, or clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition that is often treated with systemic corticosteroid therapy. These events usually, but not always, have been associated with the reduction of oral steroid therapy. Be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy in patients.
Concurrent corticosteroids: While the dose of inhaled corticosteroid may be reduced gradually under medical supervision, do not abruptly substituted montelukast for inhaled or oral corticosteroids.
Aspirin sensitivity: Inform patients with known aspirin sensitivity that they should continue avoidance of aspirin or anti-inflammatory drugs (NSAIDs) while taking montelukast. Although montelukast is effective in improving airway function in asthmatic patients with documented aspirin sensitivity, it has not been shown to truncate bronchoconstrictor response to aspirin and other NSAIDs drugs in aspirin-sensitive asthmatic patients.

Pregnancy: Pregnancy category B. Adverse events have not been observed in animal reproduction studies with montelukast. Based on available data, an increased risk of teratogenic effects has not been observed with montelukast use in pregnancy.
Lactation: It is not known if montelukast is excreted in human milk. Exercise caution when montelukast is given to a breast feeding mother.

Central nervous system: Agitation (including aggressive behavior or hostility), anxiousness, depression, disorientation, disturbance in attention, dream abnormalities, drowsiness, hallucinations, hypesthesia, insomnia, irritability, memory impairment, paresthesia, restlessness, seizures, somnambulism, suicidal thinking and behavior (including suicide), tremor.
Dermatologic: Erythema multiforme, erythema nodosum, pruritus, Stevens-Johnson syndrome/toxic epidermal necrolysis, urticaria.
Gastrointestinal: Diarrhea, dyspepsia, nausea, pancreatitis, vomiting.
Hematologic: Increased bleeding tendency, systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, thrombocytopenia.
Hepatic: Cholestatic hepatitis, hepatocellular liver injury, mixed-pattern liver injury.
Hypersensitivity: Angioedema, hypersensitivity reactions, including anaphylaxis.
Musculoskeletal: Arthralgia, myalgia (including muscle cramps).
Miscellaneous: Bruising, edema, enuresis in children, epistaxis, hepatic eosinophilic infiltration, palpitations, pulmonary eosinophilia.

Montelukast is the substrate of CYP2C8 (minor), CYP2C9 (minor), CYP3A4 (minor). Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Montelukast inhibits CYP2C8 (weak), CYP2C9 (weak).
Avoid concomitant use of Montelukast with Loxapine.
Montelukast may increase the levels/effects of Loxapine.
The levels/effects of Montelukast may be increased by Gemfibrozil.
The levels/effects of Montelukast may be decreased by Lumacaftor.

Store below 30°C. Protect from moisture and light.

Antiasthmatic & COPD Preparations

R03DC03 - montelukast ; Belongs to the class of leukotriene receptor antagonists. Used in the systemic treatment of obstructive airway diseases.

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